US2011039899A1PendingUtilityA1
Gabapentin for the Treatment of Overactive Bladder, Stress Incontinence and BPH
Est. expiryDec 13, 2022(expired)· nominal 20-yr term from priority
A61K 31/198A61K 31/401A61K 31/16A61K 31/197A61K 31/662A61K 31/20A61K 31/4015A61K 31/41A61K 31/4245A61K 31/185A61K 31/433A61K 45/06A61K 31/18A61K 31/195A61P 13/00
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Claims
Abstract
Use of an alpha-2-delta ligand, or a pharmaceutically acceptable derivative thereof, for the manufacture of a medicament for the treatment of LUTS, other than urinary incontinence, associated with OAB and/or BPH.
Claims
exact text as granted — not AI-modified1 . A method of treating LUTS, other than urinary incontinence, associated with OAB and/or BPH comprising administering an alpha-2-delta ligand, or a pharmaceutically acceptable salt or solvate thereof, to a patient in need of such treatment.
2 . The method of claim 1 , wherein the LUTS is associated with BPH.
3 . The method of claim 1 , wherein the LUTS is associated with OAB.
4 . The method of claim 3 , wherein the OAB is OAB dry.
5 . The method of claim 1 , wherein the LUTS is frequency.
6 . The method of claim 1 , wherein the LUTS is nocturia.
7 . The method of claim 1 , wherein the alpha-2-delta ligand is selected from the group consisting of:
or a pharmaceutically acceptable salt or solvate thereof;
wherein R 1 and R 2 are each independently selected from H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, phenyl and benzyl, subject to the proviso that, except in the case of a tricyclooctane compound of formula (XVIII), R 1 and R 2 are not simultaneously hydrogen; or it is selected from the group consisting of:
or a pharmaceutically acceptable salt or solvate thereof.
8 . The method of claim 7 wherein the alpha-2-delta ligand is gabapentin (I)
or a pharmaceutically acceptable salt or solvate thereof.
9 . The method of claim 7 wherein the alpha-2-delta ligand is pregabalin (II)
or a pharmaceutically acceptable salt or solvate thereof.
10 . The method of claim 1 wherein the alpha-2-delta ligand is (1α,3α,5α)(3-amino-methyl-bicyclo[3.2.0]hept-3-yl)-acetic acid (III′)
or a pharmaceutically acceptable salt or solvate thereof.
11 . The method of claim 7 , wherein the alpha-2-delta ligand is 4-(3-fluoro-benzyl)-pyrrolidine-2-carboxylic acid (XXXV)
or a pharmaceutically acceptable salt or solvate thereof.
12 . The method of claim 7 , wherein the alpha-2-delta ligand is a compound of formula (XXX) as defined therein, or a pharmaceutically acceptable salt or solvate thereof.
13 . A method of treating LUTS associated with OAB and/or BPH comprising administering to a patient in need of such treatment a combination of an alpha-2-delta ligand and a compound selected from the group consisting of:
(i) a PDEV inhibitory compound; and (ii) a muscarinic antagonist;
or pharmaceutically acceptable salts or solvates thereof.
14 . The method of claim 13 , wherein the alpha-2-delta ligand is administered in combination with a muscarinic antagonist.
15 . The method of claim 14 , wherein the muscarinic antagonist is tolterodine.
16 . The method of claim 13 , wherein the LUTS is other than urinary incontinence.
17 . The method of claim 13 , wherein the LUTS is associated with BPH.
18 . The method of claim 13 , wherein the LUTS is associated with OAB.
19 . The method of claim 18 , wherein the OAB is OAB dry.
20 . The method of claim 13 , wherein the LUTS is frequency.
21 . The method of claim 13 , wherein the LUTS is nocturia.
22 . The method of claim 13 , wherein the alpha-2-delta ligand is selected from the group consisting of:
or a pharmaceutically acceptable salt or solvate thereof;
wherein R 1 and R 2 are each independently selected from H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, phenyl and benzyl, subject to the proviso that, except in the case of a tricyclooctane compound of formula (XVIII), R 1 and R 2 are not simultaneously hydrogen; or it is selected from the group consisting of:
or a pharmaceutically acceptable salt or solvate thereof.
23 . The method of claim 22 wherein the alpha-2-delta ligand is gabapentin (I)
or a pharmaceutically acceptable salt or solvate thereof.
24 . The method of claim 22 wherein the alpha-2-delta ligand is pregabalin (II)
or a pharmaceutically acceptable salt or solvate thereof.
25 . The method of claim 13 wherein the alpha-2-delta ligand is (1α,3α,5α)(3-amino-methyl-bicyclo[3.2.0]hept-3-yl)-acetic acid (III′)
or a pharmaceutically acceptable salt or solvate thereof.
26 . The method of claim 22 , wherein the alpha-2-delta ligand is 4-(3-fluoro-benzyl)-pyrrolidine-2-carboxylic acid (XXXV)
or a pharmaceutically acceptable salt or solvate thereof.
27 . The method of claim 22 , wherein the alpha-2-delta ligand is a compound of formula (XXX) as defined therein, or a pharmaceutically acceptable salt or solvate thereof.
28 . A pharmaceutical composition containing an alpha-2-delta ligand and a compound selected from the group consisting of:
(i) a PDEV inhibitor; and (ii) a muscarinic antagonist;
or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier.
29 . The pharmaceutical composition of claim 28 , wherein the alpha-2-delta ligand is selected from the group consisting of:
or a pharmaceutically acceptable salt or solvate thereof;
wherein R 1 and R 2 are each independently selected from H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, phenyl and benzyl, subject to the proviso that, except in the case of a tricyclooctane compound of formula (XVIII), R 1 and R 2 are not simultaneously hydrogen; or it is selected from the group consisting of:
or a pharmaceutically acceptable salt or solvate thereof, and is in combination with a muscarinic antagonist.
30 . The pharmaceutical composition of claim 29 , wherein the muscarinic antagonist is tolterodine.Join the waitlist — get patent alerts
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